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Thapsigargin Epoxide

A Nonactive Analogue of Thapsigargin
Cat #: T-670
Lyophilized Powder yes
Origin Thapsia garganica.
Source Natural
MW: 632.75
Purity: >99%
Effective concentration 100 nM.
Structure
Molecular formula C34H48O11.
Activity Thapsigargin is an extremely tight-binding inhibitor of intracellular Ca2+ pumps, but initially described as a tumor promoting agent which induces rapid Ca2+ release from intracellular stores1. Thapsigargin epoxide is a non-active analogue of Thapsigargin.
References-Activity
  1. Norup, E. et al. (1986) Planta. Med. 4, 251.
  2. Jackson, T.R. et al. (1988) Biochem. J253, 81.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility DMSO, ethanol, acetone or methanol. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to one week at 4°C or six months at -20°C.
References - Scientific background
  1. Elison, C. and Jenden, D.J. (1967) Biochem. Pharmacol. 16, 1347.
  2. Frank, M. and Sleaton, W.W. (1975) Res. Commun. Chem. Pathol. Pharmacol. 11, 65.
  3. Lai, F.A. et al. (1989) J. Biol. Chem. 264, 16776.
  4. Lai, F.A. et al. (1988) Nature 331, 315.
  5. Tu, Q. et al. (1994) Biophys. J. 67, 2280.
  6. Buck, E. et al. (1992) J. Biol. Chem. 267, 23560.
  7. Ogawa, Y. (1994) Crit. Rev. Biochem. Mol. Biol. 29, 229.
  8. Chu, A. et al. (1990) Mol Pharmacol. 37, 735.
  9. Norup, E. et al. (1986) Planta. Med. 4, 251.
  10. Jackson, T.R. et al. (1988) Biochem. J. 253, 81.
Scientific background

Thapsigargin, derived from the plant genus Thapsia1,2, is an extremely tight-binding inhibitor of intracellular Ca2+ pumps. It was initially described as a tumor promoting agent that induces rapid Ca2+ release from intracellular stores3 by the inhibition of the sarcoplasmic endoplasmic reticulm Ca2+-dependent ATPase pump without inositol phosphate formation4. Thapsigargin-induced depletion of Ca2+ stores causes apoptosis in most cell lines5. It has also been shown to cause histamine secretion from rat mast cells6 and to stimulate arachidonic acid metabolism in macrophages7. Its tumour-promoting function probably results, at least partly, from cytotoxicity, causing a wound response in the skin8.

Thapsigargin Epoxide is a non-active analogue of Thapsigargin and can be used as a negative control for Thapsigargin activity9,10.

Target SERCA
Last update: 16/08/2020

Thapsigargin Epoxide (#T-670) is a highly pure, natural, and biologically active compound.

For research purposes only, not for human use
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